Synonyms:hydroimidazolone;imidazolone
≥95% *data from raw suppliers
IMIDAZOLONE 95.00% *data from reagent suppliers
The study focuses on the design, synthesis, and evaluation of hydrophilic bisazole analogs as potential correctors for the most common cystic fibrosis (CF) mutation, the deletion of phenylalanine residue 508 in the CF transmembrane regulator conductance (CFTR) protein. The aim is to develop small molecules that can correct the misfolding of defective DF508-CFTR, which is retained in the endoplasmic reticulum and rapidly degraded, leading to impaired chloride transport and the associated symptoms of CF. The researchers synthesized and tested five more hydrophilic bisazole analogs of a previously identified bithiazole CF corrector, with the goal of identifying new CFTR correctors with less hydrophobicity and potentially increased hydrophilicity and stronger hydrogen bonding interactions within the DF508-CFTR binding site. The chemicals used in the study include various bisazole derivatives such as thiazole-tethered imidazolones, oxazoles, oxadiazoles, and thiadiazoles, which were designed to replace one of the two thiazole rings in the lead compound to explore different chemotypes and improve the drug's pharmacokinetic properties. The purpose of these chemicals was to assess their DF508-CFTR corrector activity and to understand the structure-activity relationships within this series of bisazoles.
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